CA2546476C - Preparation pharmaceutique comprenant de la gabapentine - Google Patents
Preparation pharmaceutique comprenant de la gabapentine Download PDFInfo
- Publication number
- CA2546476C CA2546476C CA2546476A CA2546476A CA2546476C CA 2546476 C CA2546476 C CA 2546476C CA 2546476 A CA2546476 A CA 2546476A CA 2546476 A CA2546476 A CA 2546476A CA 2546476 C CA2546476 C CA 2546476C
- Authority
- CA
- Canada
- Prior art keywords
- gabapentin
- granulate
- weight
- pharmaceutical composition
- additives
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired - Lifetime
Links
- UGJMXCAKCUNAIE-UHFFFAOYSA-N Gabapentin Chemical compound OC(=O)CC1(CN)CCCCC1 UGJMXCAKCUNAIE-UHFFFAOYSA-N 0.000 title claims abstract description 124
- 229960002870 gabapentin Drugs 0.000 title claims abstract description 61
- 239000000825 pharmaceutical preparation Substances 0.000 title description 2
- 239000008187 granular material Substances 0.000 claims abstract description 56
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract description 15
- 238000002844 melting Methods 0.000 claims abstract description 11
- 230000008018 melting Effects 0.000 claims abstract description 11
- 239000000654 additive Substances 0.000 claims description 25
- 239000002775 capsule Substances 0.000 claims description 20
- 239000000203 mixture Substances 0.000 claims description 18
- 238000002360 preparation method Methods 0.000 claims description 8
- 150000003951 lactams Chemical class 0.000 claims description 7
- 239000007787 solid Substances 0.000 claims description 5
- 239000001828 Gelatine Substances 0.000 claims description 4
- 229920000159 gelatin Polymers 0.000 claims description 4
- 235000019322 gelatine Nutrition 0.000 claims description 4
- 239000012535 impurity Substances 0.000 claims description 4
- 239000000126 substance Substances 0.000 claims description 4
- 239000003085 diluting agent Substances 0.000 claims description 3
- 239000000314 lubricant Substances 0.000 claims description 3
- 239000007884 disintegrant Substances 0.000 claims 2
- 229920001223 polyethylene glycol Polymers 0.000 description 18
- 239000002202 Polyethylene glycol Substances 0.000 description 17
- GWEVSGVZZGPLCZ-UHFFFAOYSA-N Titan oxide Chemical compound O=[Ti]=O GWEVSGVZZGPLCZ-UHFFFAOYSA-N 0.000 description 10
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 7
- 229920002785 Croscarmellose sodium Polymers 0.000 description 5
- 229920000881 Modified starch Polymers 0.000 description 5
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 description 5
- 239000008119 colloidal silica Substances 0.000 description 5
- 229960001681 croscarmellose sodium Drugs 0.000 description 5
- 235000010947 crosslinked sodium carboxy methyl cellulose Nutrition 0.000 description 5
- 239000004408 titanium dioxide Substances 0.000 description 5
- 239000002253 acid Substances 0.000 description 4
- 150000001450 anions Chemical class 0.000 description 4
- UKMSUNONTOPOIO-UHFFFAOYSA-N docosanoic acid Chemical compound CCCCCCCCCCCCCCCCCCCCCC(O)=O UKMSUNONTOPOIO-UHFFFAOYSA-N 0.000 description 4
- 239000003814 drug Substances 0.000 description 4
- 229910052500 inorganic mineral Inorganic materials 0.000 description 4
- 239000007788 liquid Substances 0.000 description 4
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 4
- 238000000034 method Methods 0.000 description 4
- 239000011707 mineral Substances 0.000 description 4
- 229920001030 Polyethylene Glycol 4000 Polymers 0.000 description 3
- 230000015556 catabolic process Effects 0.000 description 3
- 238000007906 compression Methods 0.000 description 3
- 230000006835 compression Effects 0.000 description 3
- 229920001577 copolymer Polymers 0.000 description 3
- 238000006731 degradation reaction Methods 0.000 description 3
- 229940079593 drug Drugs 0.000 description 3
- 238000005469 granulation Methods 0.000 description 3
- 230000003179 granulation Effects 0.000 description 3
- 150000002735 metacrylic acids Chemical class 0.000 description 3
- 239000000843 powder Substances 0.000 description 3
- 235000021357 Behenic acid Nutrition 0.000 description 2
- 229920002261 Corn starch Polymers 0.000 description 2
- 150000007513 acids Chemical class 0.000 description 2
- 150000001298 alcohols Chemical class 0.000 description 2
- 229940116226 behenic acid Drugs 0.000 description 2
- 230000015572 biosynthetic process Effects 0.000 description 2
- 239000008120 corn starch Substances 0.000 description 2
- 229940099112 cornstarch Drugs 0.000 description 2
- 150000002148 esters Chemical class 0.000 description 2
- 239000000741 silica gel Substances 0.000 description 2
- 229910002027 silica gel Inorganic materials 0.000 description 2
- 239000003381 stabilizer Substances 0.000 description 2
- 238000003756 stirring Methods 0.000 description 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 2
- 238000005079 FT-Raman Methods 0.000 description 1
- 239000008118 PEG 6000 Substances 0.000 description 1
- 229920002535 Polyethylene Glycol 1500 Polymers 0.000 description 1
- 229920002584 Polyethylene Glycol 6000 Polymers 0.000 description 1
- 150000001299 aldehydes Chemical class 0.000 description 1
- 238000004458 analytical method Methods 0.000 description 1
- 239000003957 anion exchange resin Substances 0.000 description 1
- 230000003556 anti-epileptic effect Effects 0.000 description 1
- 239000003963 antioxidant agent Substances 0.000 description 1
- 229940116224 behenate Drugs 0.000 description 1
- UKMSUNONTOPOIO-UHFFFAOYSA-M behenate Chemical compound CCCCCCCCCCCCCCCCCCCCCC([O-])=O UKMSUNONTOPOIO-UHFFFAOYSA-M 0.000 description 1
- 239000011248 coating agent Substances 0.000 description 1
- 238000000576 coating method Methods 0.000 description 1
- 150000001875 compounds Chemical class 0.000 description 1
- 239000007857 degradation product Substances 0.000 description 1
- 230000018044 dehydration Effects 0.000 description 1
- 238000006297 dehydration reaction Methods 0.000 description 1
- 230000000368 destabilizing effect Effects 0.000 description 1
- 238000007907 direct compression Methods 0.000 description 1
- 238000009776 industrial production Methods 0.000 description 1
- 150000002576 ketones Chemical class 0.000 description 1
- 239000000463 material Substances 0.000 description 1
- 239000003960 organic solvent Substances 0.000 description 1
- 239000000047 product Substances 0.000 description 1
- 239000002994 raw material Substances 0.000 description 1
- 239000004094 surface-active agent Substances 0.000 description 1
- VUYXVWGKCKTUMF-UHFFFAOYSA-N tetratriacontaethylene glycol monomethyl ether Chemical compound COCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCO VUYXVWGKCKTUMF-UHFFFAOYSA-N 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 231100000331 toxic Toxicity 0.000 description 1
- 230000002588 toxic effect Effects 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1629—Organic macromolecular compounds
- A61K9/1641—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poloxamers
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
- A61K9/2077—Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/08—Antiepileptics; Anticonvulsants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/08—Antiepileptics; Anticonvulsants
- A61P25/10—Antiepileptics; Anticonvulsants for petit-mal
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/08—Antiepileptics; Anticonvulsants
- A61P25/12—Antiepileptics; Anticonvulsants for grand-mal
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pain & Pain Management (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicinal Preparation (AREA)
Abstract
L'invention concerne un granulé de gabapentine obtenu par granulation de la gabapentine avec PEG possédant un point de fusion compris entre 50 et 80 ·C et des compostions pharmaceutiques renfermant celui-ci.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IT002399A ITMI20032399A1 (it) | 2003-12-09 | 2003-12-09 | Composizione farmaceutica contenente gabapentina. |
| ITMI2003A002399 | 2003-12-09 | ||
| PCT/EP2004/053233 WO2005055993A2 (fr) | 2003-12-09 | 2004-12-02 | Preparation pharmaceutique comprenant de la gabapentine |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CA2546476A1 CA2546476A1 (fr) | 2005-06-23 |
| CA2546476C true CA2546476C (fr) | 2012-01-31 |
Family
ID=34674559
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA2546476A Expired - Lifetime CA2546476C (fr) | 2003-12-09 | 2004-12-02 | Preparation pharmaceutique comprenant de la gabapentine |
Country Status (21)
| Country | Link |
|---|---|
| US (2) | US20080194687A1 (fr) |
| EP (1) | EP1699438B1 (fr) |
| JP (1) | JP5432433B2 (fr) |
| CN (1) | CN100508966C (fr) |
| AT (1) | ATE506052T1 (fr) |
| AU (1) | AU2004296561B2 (fr) |
| BR (1) | BRPI0417420B1 (fr) |
| CA (1) | CA2546476C (fr) |
| DE (1) | DE602004032382D1 (fr) |
| DK (1) | DK1699438T3 (fr) |
| EA (1) | EA012068B1 (fr) |
| ES (1) | ES2363503T3 (fr) |
| HR (1) | HRP20110346T1 (fr) |
| IL (1) | IL175764A (fr) |
| IT (1) | ITMI20032399A1 (fr) |
| NZ (1) | NZ547764A (fr) |
| PL (1) | PL1699438T3 (fr) |
| PT (1) | PT1699438E (fr) |
| SI (1) | SI1699438T1 (fr) |
| WO (1) | WO2005055993A2 (fr) |
| ZA (1) | ZA200604717B (fr) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| USD663617S1 (en) | 2010-01-14 | 2012-07-17 | S.C. Johnson & Son, Inc. | Container with nozzle |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8607620B2 (en) * | 2007-10-02 | 2013-12-17 | Shimadzu Corporation | Preparative separation/purification system |
| KR20190003805A (ko) * | 2016-05-27 | 2019-01-09 | 한미약품 주식회사 | 암 세포 성장을 저해하는 아민 유도체 또는 이의 약학적으로 허용가능한 염 및 저융점을 갖는 안정화제를 포함하는 약학적 조성물 |
| RU2731536C1 (ru) * | 2019-07-30 | 2020-09-04 | Общество С Ограниченной Ответственностью "Консорциум-Пик" | Фармацевтические композиции, содержащие фенозановую кислоту |
| RU2736479C1 (ru) * | 2019-07-30 | 2020-11-17 | Общество С Ограниченной Ответственностью "Консорциум-Пик" | Не содержащая наполнитель фармацевтическая композиция, содержащая фенозановую кислоту |
Family Cites Families (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BE621097A (fr) * | 1961-08-05 | |||
| US3147187A (en) * | 1962-09-10 | 1964-09-01 | Don Hall Lab | Sustained release pharmaceutical |
| JPS58214333A (ja) * | 1982-06-04 | 1983-12-13 | Dai Ichi Seiyaku Co Ltd | 粒状物 |
| US4443428A (en) * | 1982-06-21 | 1984-04-17 | Euroceltique, S.A. | Extended action controlled release compositions |
| US5169645A (en) * | 1989-10-31 | 1992-12-08 | Duquesne University Of The Holy Ghost | Directly compressible granules having improved flow properties |
| US5078990A (en) * | 1990-07-13 | 1992-01-07 | Helene Curtis, Inc. | Shampoos and conditioning shampoos having increased capacity for incorporation of conditioning agents and removal of hair soil |
| US5232704A (en) * | 1990-12-19 | 1993-08-03 | G. D. Searle & Co. | Sustained release, bilayer buoyant dosage form |
| US5429825A (en) * | 1992-06-26 | 1995-07-04 | Mcneil-Ppc, Inc. | Rotomelt granulation |
| EP0818990A1 (fr) * | 1995-04-03 | 1998-01-21 | Abbott Laboratories | Melanges homogenes de medicaments fondant a basse temperature et d'additifs, destines a une liberation lente |
| CA2302275C (fr) * | 1997-09-19 | 2009-12-08 | Shire Laboratories, Inc. | Granule de solution solide |
| ID26395A (id) * | 1998-05-15 | 2000-12-21 | Warner Lambert Comapny | Turunan asam gamma-aminobutirat yang mengandung komposisi padat dan proses pembuatannya |
| IL125244A (en) | 1998-07-07 | 2002-12-01 | Yissum Res Dev Co | Pharmaceutical compositions containing low-melting waxes |
| FR2781793B1 (fr) * | 1998-08-03 | 2001-07-20 | Prographarm Lab | Procede de fabrication de granules de gabapentine enrobes |
| US6248363B1 (en) * | 1999-11-23 | 2001-06-19 | Lipocine, Inc. | Solid carriers for improved delivery of active ingredients in pharmaceutical compositions |
| US7374779B2 (en) | 1999-02-26 | 2008-05-20 | Lipocine, Inc. | Pharmaceutical formulations and systems for improved absorption and multistage release of active agents |
| US20020015730A1 (en) * | 2000-03-09 | 2002-02-07 | Torsten Hoffmann | Pharmaceutical formulations and method for making |
| US7056951B2 (en) * | 2000-09-26 | 2006-06-06 | Mutual Pharmaceutical Co., Inc. | Stable solid dosage forms of amino acids and processes for producing same |
| DE60211769T2 (de) * | 2001-03-07 | 2007-05-24 | Dainippon Sumitomo Pharma Co., Ltd. | Verfahren zur Herstellung von Arzneistoffgranulatkörnern, die Arzneistoffgranulatkörner sowie diese enthaltende pharmazeutische Zubereitungen |
| ITMI20011337A1 (it) | 2001-06-26 | 2002-12-26 | Farmatron Ltd | Composizioni farmaceutiche orali a rilascio modificato del principio attivo |
| TWI312285B (en) * | 2001-10-25 | 2009-07-21 | Depomed Inc | Methods of treatment using a gastric retained gabapentin dosage |
| WO2003082804A1 (fr) | 2002-03-28 | 2003-10-09 | Synthon B.V. | Besylate de venlafaxine |
| CN1720025A (zh) * | 2002-10-08 | 2006-01-11 | 兰贝克赛实验室有限公司 | 加巴喷丁片剂及其制备 |
-
2003
- 2003-12-09 IT IT002399A patent/ITMI20032399A1/it unknown
-
2004
- 2004-12-02 NZ NZ547764A patent/NZ547764A/en not_active IP Right Cessation
- 2004-12-02 DE DE602004032382T patent/DE602004032382D1/de not_active Expired - Lifetime
- 2004-12-02 DK DK04804655.1T patent/DK1699438T3/da active
- 2004-12-02 AT AT04804655T patent/ATE506052T1/de active
- 2004-12-02 PL PL04804655T patent/PL1699438T3/pl unknown
- 2004-12-02 SI SI200431665T patent/SI1699438T1/sl unknown
- 2004-12-02 EA EA200600939A patent/EA012068B1/ru unknown
- 2004-12-02 EP EP04804655A patent/EP1699438B1/fr not_active Expired - Lifetime
- 2004-12-02 JP JP2006543535A patent/JP5432433B2/ja not_active Expired - Lifetime
- 2004-12-02 WO PCT/EP2004/053233 patent/WO2005055993A2/fr not_active Ceased
- 2004-12-02 AU AU2004296561A patent/AU2004296561B2/en not_active Expired
- 2004-12-02 US US10/581,367 patent/US20080194687A1/en not_active Abandoned
- 2004-12-02 PT PT04804655T patent/PT1699438E/pt unknown
- 2004-12-02 CN CNB2004800366347A patent/CN100508966C/zh not_active Expired - Lifetime
- 2004-12-02 BR BRPI0417420-8A patent/BRPI0417420B1/pt not_active IP Right Cessation
- 2004-12-02 ES ES04804655T patent/ES2363503T3/es not_active Expired - Lifetime
- 2004-12-02 CA CA2546476A patent/CA2546476C/fr not_active Expired - Lifetime
- 2004-12-02 HR HR20110346T patent/HRP20110346T1/hr unknown
-
2006
- 2006-05-18 IL IL175764A patent/IL175764A/en active IP Right Grant
- 2006-06-08 ZA ZA200604717A patent/ZA200604717B/xx unknown
-
2011
- 2011-04-06 US US13/081,036 patent/US8927017B2/en not_active Expired - Lifetime
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| USD663617S1 (en) | 2010-01-14 | 2012-07-17 | S.C. Johnson & Son, Inc. | Container with nozzle |
Also Published As
| Publication number | Publication date |
|---|---|
| JP5432433B2 (ja) | 2014-03-05 |
| ATE506052T1 (de) | 2011-05-15 |
| CN100508966C (zh) | 2009-07-08 |
| EA200600939A1 (ru) | 2006-12-29 |
| EP1699438B1 (fr) | 2011-04-20 |
| IL175764A (en) | 2012-08-30 |
| ITMI20032399A1 (it) | 2005-06-10 |
| EA012068B1 (ru) | 2009-08-28 |
| SI1699438T1 (sl) | 2011-09-30 |
| JP2007513920A (ja) | 2007-05-31 |
| ZA200604717B (en) | 2007-03-28 |
| DE602004032382D1 (de) | 2011-06-01 |
| IL175764A0 (en) | 2008-04-13 |
| DK1699438T3 (da) | 2011-08-15 |
| BRPI0417420B1 (pt) | 2021-10-13 |
| WO2005055993A2 (fr) | 2005-06-23 |
| AU2004296561B2 (en) | 2009-02-26 |
| CA2546476A1 (fr) | 2005-06-23 |
| ES2363503T3 (es) | 2011-08-05 |
| US8927017B2 (en) | 2015-01-06 |
| AU2004296561A1 (en) | 2005-06-23 |
| HRP20110346T1 (hr) | 2011-06-30 |
| WO2005055993A3 (fr) | 2006-05-26 |
| EP1699438A2 (fr) | 2006-09-13 |
| BRPI0417420A (pt) | 2007-03-06 |
| PT1699438E (pt) | 2011-07-05 |
| CN1889934A (zh) | 2007-01-03 |
| NZ547764A (en) | 2009-09-25 |
| US20110189272A1 (en) | 2011-08-04 |
| US20080194687A1 (en) | 2008-08-14 |
| PL1699438T3 (pl) | 2011-10-31 |
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| BG99078A (en) | Preparation having controllable release |
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